• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

新型组蛋白去乙酰化酶抑制剂噻唑-5-异羟肟酸的设计与合成

Design and synthesis of thiazole-5-hydroxamic acids as novel histone deacetylase inhibitors.

作者信息

Anandan Sampath-Kumar, Ward John S, Brokx Richard D, Denny Trisha, Bray Mark R, Patel Dinesh V, Xiao Xiao-Yi

机构信息

EntreMed Inc., 101 College Street, Toronto Medical Discovery Tower, Toronto, Ontario, Canada M5G1L7.

出版信息

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5995-9. doi: 10.1016/j.bmcl.2007.07.050. Epub 2007 Aug 19.

DOI:10.1016/j.bmcl.2007.07.050
PMID:17827005
Abstract

We have designed and synthesized a series of structurally novel hydroxamic acid-based histone deacetylase (HDAC) inhibitors characterized by a zinc chelating head group attached directly to a thiazole ring. The thiazole ring connects to a piperazine spacer, which is capped with a sulfonamide group. These novel molecules potently inhibit an HDAC enzyme mixture derived from HeLa cervical carcinoma cells and show potent antiproliferative activity against the breast cancer cell line MCF7.

摘要

我们设计并合成了一系列结构新颖的基于异羟肟酸的组蛋白去乙酰化酶（HDAC）抑制剂，其特征在于直接连接到噻唑环上的锌螯合头部基团。噻唑环连接到哌嗪间隔基，该间隔基由磺酰胺基团封端。这些新型分子能有效抑制源自人宫颈癌HeLa细胞的HDAC酶混合物，并对乳腺癌细胞系MCF7显示出强大的抗增殖活性。

相似文献

1
Design and synthesis of thiazole-5-hydroxamic acids as novel histone deacetylase inhibitors.新型组蛋白去乙酰化酶抑制剂噻唑-5-异羟肟酸的设计与合成
Bioorg Med Chem Lett. 2007 Nov 1;17(21):5995-9. doi: 10.1016/j.bmcl.2007.07.050. Epub 2007 Aug 19.
2
Design and synthesis of non-hydroxamate histone deacetylase inhibitors: identification of a selective histone acetylating agent.非异羟肟酸类组蛋白去乙酰化酶抑制剂的设计与合成：一种选择性组蛋白乙酰化剂的鉴定
Bioorg Med Chem. 2005 Jul 1;13(13):4332-42. doi: 10.1016/j.bmc.2005.04.002.
3
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.潜在抗肿瘤药物的研发。一组新型磺胺类衍生物作为组蛋白去乙酰化酶抑制剂的合成及生物学评价。
J Med Chem. 2003 Feb 27;46(5):820-30. doi: 10.1021/jm020377a.
4
Discovery of pyrimidyl-5-hydroxamic acids as new potent histone deacetylase inhibitors.嘧啶基-5-异羟肟酸作为新型强效组蛋白去乙酰化酶抑制剂的发现。
Eur J Med Chem. 2005 Jun;40(6):597-606. doi: 10.1016/j.ejmech.2005.01.008. Epub 2005 Mar 3.
5
Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.异吲哚啉酮-异羟肟酸衍生物作为组蛋白去乙酰化酶（HDAC）抑制剂的设计、合成与评价
Bioorg Med Chem Lett. 2007 Sep 1;17(17):4895-900. doi: 10.1016/j.bmcl.2007.06.038. Epub 2007 Jun 13.
6
Design, synthesis, and evaluation of cyclic amide/imide-bearing hydroxamic acid derivatives as class-selective histone deacetylase (HDAC) inhibitors.含环酰胺/酰亚胺的异羟肟酸衍生物作为类别选择性组蛋白脱乙酰酶（HDAC）抑制剂的设计、合成与评价
Bioorg Med Chem. 2006 Nov 15;14(22):7625-51. doi: 10.1016/j.bmc.2006.07.008. Epub 2006 Jul 31.
7
Synthesis of rigid trichostatin A analogs as HDAC inhibitors.作为组蛋白去乙酰化酶抑制剂的刚性曲古抑菌素A类似物的合成。
Bioorg Med Chem Lett. 2006 Oct 15;16(20):5339-44. doi: 10.1016/j.bmcl.2006.07.080. Epub 2006 Aug 14.
8
Exploring bis-(indolyl)methane moiety as an alternative and innovative CAP group in the design of histone deacetylase (HDAC) inhibitors.在组蛋白去乙酰化酶（HDAC）抑制剂设计中探索双（吲哚基）甲烷部分作为一种替代且创新的封端基团。
Bioorg Med Chem Lett. 2009 May 15;19(10):2840-3. doi: 10.1016/j.bmcl.2009.03.101. Epub 2009 Mar 26.
9
Design and synthesis of aryl ether and sulfone hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.芳基醚和砜羟肟酸的设计与合成作为有效的组蛋白去乙酰化酶（HDAC）抑制剂。
Bioorg Med Chem Lett. 2011 Jan 1;21(1):324-8. doi: 10.1016/j.bmcl.2010.11.006. Epub 2010 Nov 5.
10
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
Eur J Med Chem. 2009 May;44(5):1900-12. doi: 10.1016/j.ejmech.2008.11.005. Epub 2008 Nov 19.

引用本文的文献

1
The Emerging Role of Histone Deacetylase Inhibitors in Cervical Cancer Therapy.组蛋白去乙酰化酶抑制剂在宫颈癌治疗中的新兴作用
Cancers (Basel). 2023 Apr 10;15(8):2222. doi: 10.3390/cancers15082222.
2
Hydroxamic acid - A novel molecule for anticancer therapy.异羟肟酸——一种用于抗癌治疗的新型分子。
J Adv Pharm Technol Res. 2012 Apr;3(2):92-9. doi: 10.4103/2231-4040.97281.
3
Regioselective synthesis of new 2-(E)-cyano(thiazolidin-2-ylidene)thiazoles.新型 2-(E)-氰基(噻唑烷-2-亚基)噻唑的区域选择性合成。
Molecules. 2009 Nov 25;14(12):4849-57. doi: 10.3390/molecules14114849.
4
A one-pot synthesis of functionalized thiazoles from acid chlorides, secondary amines, ethyl bromopyruvate, and ammonium thiocyanate.由酰氯、仲胺、溴丙酮酸乙酯和硫氰酸铵一锅法合成功能化噻唑。
Mol Divers. 2009 Aug;13(3):295-300. doi: 10.1007/s11030-009-9114-3. Epub 2009 Feb 10.